Mahboobi Siavosh, Eichhorn Emerich, Popp Alfred, Sellmer Andreas, Elz Sigurd, Möllmann Ute
Department of Pharmaceutical Chemistry I, University of Regensburg, D-93040 Regensburg, Germany.
Eur J Med Chem. 2006 Feb;41(2):176-91. doi: 10.1016/j.ejmech.2005.10.006. Epub 2006 Jan 10.
A number of new compounds containing 3-bromo-2,5-dihydro-1H-2,5-pyrroledione and indole substructures were found to have antibacterial activity against resistant strains of Staphylococcus aureus, Mycobacterium smegmatis and some other Gram positive bacteria. The investigated compounds exhibit minimal inhibition concentrations (MIC's) lower than those of ciprofloxacin, vancomycin and doxycycline resp. A different spectrum of activity, suggests a mechanism of action different to vancomycin and doxycycline. This might be important in circumventing existing resistance mechanisms. Here we report about the synthesis and on the antibacterial activity in a structure activity relationship study.
发现许多含有3-溴-2,5-二氢-1H-2,5-吡咯二酮和吲哚亚结构的新化合物对金黄色葡萄球菌、耻垢分枝杆菌和其他一些革兰氏阳性菌的耐药菌株具有抗菌活性。所研究的化合物表现出的最低抑菌浓度（MIC）分别低于环丙沙星、万古霉素和强力霉素。不同的活性谱表明其作用机制与万古霉素和强力霉素不同。这在规避现有耐药机制方面可能很重要。在此，我们报告在一项构效关系研究中的合成及抗菌活性情况。
